Abstract

The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. The full contents can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.13350/full. Voltage‐gated ion channels are one of the eight major pharmacological targets into which the Guide is divided, with the others being: G protein‐coupled receptors, ligand‐gated ion channels, other ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The Concise Guide is published in landscape format in order to facilitate comparison of related targets. It is a condensed version of material contemporary to late 2015, which is presented in greater detail and constantly updated on the website www.guidetopharmacology.org, superseding data presented in the previous Guides to Receptors & Channels and the Concise Guide to PHARMACOLOGY 2013/14. It is produced in conjunction with NC‐IUPHAR and provides the official IUPHAR classification and nomenclature for human drug targets, where appropriate. It consolidates information previously curated and displayed separately in IUPHAR‐DB and GRAC and provides a permanent, citable, point‐in‐time record that will survive database updates.

Highlights

  • Stephen PH Alexander1, William A Catterall2, Eamonn Kelly3, Neil Marrion3, John A Peters4, Helen E Benson5, Elena Faccenda5, Adam J Pawson5, Joanna L Sharman5, Christopher Southan5, Jamie A Davies5 and CGTP Collaborators

  • Targeted disruption of Catsper1, 2, 3, 4, or Æ genes results in an identical phenotype in which spermatozoa fail to exhibit the hyperactive movement necessary for penetration of the egg cumulus and zona pellucida and subsequent fertilization. Such disruptions are associated with a deficit in alkalinization and depolarization-evoked Ca2 entry into spermatozoa [47, 59, 299]

  • A standardised nomenclature for Cyclic nucleotide-gated (CNG) channels has been proposed by the NC-IUPHAR subcommittee on voltage-gated ion channels [138]

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Summary

University of Dundee

The Concise Guide to PHARMACOLOGY 2015/16 Alexander, Stephen P. H.; Catterall, William A.; Kelly, Eamonn; Marrion, Neil; Peters, John A.; Benson, Helen E. Citation for published version (APA): Alexander, S. A., Kelly, E., Marrion, N., Peters, J. The Concise Guide to PHARMACOLOGY 2015/16: Voltage-gated ion channels. S.P.H. Alexander et al The Concise Guide to PHARMACOLOGY 2015/16: Voltage-gated ion channels. British Journal of Pharmacology (2015) 172, 5904–5941. Stephen PH Alexander, William A Catterall, Eamonn Kelly, Neil Marrion, John A Peters, Helen E Benson, Elena Faccenda, Adam J Pawson, Joanna L Sharman, Christopher Southan, Jamie A Davies and CGTP Collaborators

Family structure
Channel blockers Selective channel blockers
Activators Channel blockers
Further Reading
Channel blockers
Potassium channels
Inhibitors Channel blockers
Gating inhibitors Channel blockers
Inwardly rectifying potassium channels
Endogenous channel blockers
Endogenous inhibitors Gating inhibitors Endogenous channel blockers
Activators Channel blockers Comments
Selective channel blockers
Functional Characteristics Channel blockers
Transient Receptor Potential channels
Selective activators Channel blockers
Endogenous channel blockers Channel blockers
Other chemical activators Physical activators
Selective activators
Labelled ligands
Gating inhibitors Selective gating inhibitors Channel blockers
Full Text
Published version (Free)

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